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98 Cards in this Set

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Adrenocorticoid antagonists (2)
1)metyrapone
2)trilostane
Metyrapone mechanism
inhibits 11beta hydroxylase (preventing cortisol synthesis)
Trilostane mechanism
inhibits 3beta deH AND 17alpha hydroxylase (preventing cortisol synthesis)
...(2) are involved in spermatogenesis
1)seminiferous tubules
2)sertoli cells (nutrition to sperm)
Leydig or Interstitial cells fxn
testosterone production
Spermatogenesis/testosterone regulation (7)
1)Hypothalamus releases GnRH
2)GnRH hits ant. pituitary and causes it to release FSH and LH
3)LH acts at leydig cells to release testosterone
4)FSH acts @ seminiferous tubule to release inhibin and increase spermatogenesis
5)Inhibin acts at hypothalamus and ant. pituitary to decr GnRH,FSH,LH
6)Testosterone acts at hypothalamus and ant. pituitary to decr GnRH,FSH,LH
7)Testosterone also acts at seminiferous tubules to incr Inhibin and incr spermatogenesis
GnRH
gonadotropin releasing hormone
___ & ____ both MUST be present for spermatogeneis to occur
1)FSH
2)testosterone
Testosterone active metabolites and the enzymes required (2)
1)dihydrotestosterone (5alpha reductase)
2)Estradiol (aromatase)
Testosterone inactive metabolites and mechanism
1)androsterone
2)etiocholanolone

liver metabolism
Testosterone activity characteristics (2)
1)high activity as itself in ant. pituitary and hypothalamus
2)low activity as itself in most tissues
What is testosterone's most active metabolism?
dihydrotestosterone, is active in most tissues
2 groups of effects of testosterone
1)androgenic effects (puberty sexual maturity)
2)anabolic effects (puberty growth)
Androgenic effects of testosterone (7)
1)growth of internal and external genital glands
2)vocal cords incr in length and thickness
3)beard and body hair grow
4)scalp hair thins and recedes
5)skin thickness increases
6)oily sebaceous gland secretion (acne)
7)CNS effects associated w/ sexual maturity
Anabolic effects of testosterone (7)
1)+ nitrogen balance
2)protein synthesis
3)incr muscle mass
4)weight gain
5)accelerated body growth
6)bone growth
7)closure of epiphysis (growth plate--is an estradiol effect)
Absorption of Testosterone (2)
a)Good thru GI but is rapidly first pass metabolized
b)esters are injected IM and absorbed slowly for ER
How to incr activity of oral testosterone
17alkalyation b/c liver metabolizes testosterone @ the 17-OH normally
98% of testosterone is bound to...
sex-hormone binding globulin and albumin
Mechanism of testosterone in tissue (4)
1)testosterone gets into cell and is converted to dihydrotestosterone via 5alpha reductase
2)it then binds an androgen receptor
3)then it binds to DNA and acts as a transcription factor
4)biologic activity follows
Prototype of natural androgen
Testosterone propionate (Testex)
Prototype of orally active androgen
Methyltestosterone (Virilron)
Prototype of Transdermal Testosterone
Testosterone Transdermal (Testoderm)
Prototype of Anabolic steroid
oxandrolone (oxandrin)
How is a natural androgen defined?
ratio of anabolic/androgenic activity is 1/1
How is anabolic steroid defined?
ratio of anabolic/androgenic activity is 2/1 to 15/1
Primary uses of anabolic stimulation (2)
1)used after major illness, burns, chemo to reverse the atrophy caused
2)illicit use in athletics
Side effects of use of anabolic steroids (6)
1)jaundice/liver cancer
2)edema
3)testicular atrophy
4)prostate hypertrophy leading to prostate cancer
5)feminizing effects in males
6)masculinization in females
____ is observed in 80% of strength athletes due to anabolic steroids
gynecomastia
3 categories of antiandrogens
1)synthesis inhibitors
2)5alpha reductase inhibitors
3)androgen receptor antagonists
Androgen synthesis inhibitor drug
GnRH (Leuprolide)
GnRH (Leuprolide) mechanism and primary application
inhibits LH secretion to decr testosterone production

prostate cancer
5alpha reductase inhibitor mechanism and application
reduces conversion of inactive testosterone to dihydrotestosterone

prostatic hypertrophy and male pattern baldness
5alpha reductase inhibitor drug
Finasteride (proscar)
Androgen-Receptor Antagonists (2 and which is more potent)
1)Spironolactone (Aldactone)
2)Flutamide (Eulexin)****
Spironolactone mechanism and application
1)weak androgen receptor antagonist and inhibits 17alpha hydroxylase
2)hirsutism in women
Flutamide mechanism and application
NON-steroidal receptor inhibitor that binds to androgen receptor and inhibits translocation to nucleus

Prostate cancer
Flutamide works best if used w/...
Leuprolide
T/F
1. Testosterone is secreted from the Sertoli Cell
2. Testosterone is absorbed by the oral route of admin but is pharmacologically inactive
3. In most target tissues, testosterone must be metabolized to dihydrotestosterone in order to work
1.False
2.True
3.True
T/F
1. Testosterone is responsible for closure of the epiphysis in males
2. Flutamide is a steroid which inhibits 5alpha reductase
1.True
2.False
Biosynthesis steps for estradiol (1 enzyme) (5)
1)Acetate to cholesterol
2)cholesterol to progesterone
3)Progesterone to Androstenedione
4)Androstenedione to testosterone
5)testosterone to estradiol via aromatase
Secretory regulation of estradiol and progesterone (5)
1)Puberty causes cerebral cortex to stimulate the hypothalamus the release GnRH
2)GnRH stimulates ant. pituitary to release FSH & LH
3)FSH & LH inhibits hypothalamus release of GnRH
4)FSH & LH stimulates ovary to release estradiol and progesterone
5)Estradiol and progesterone inhibit ant. pituitary release of FSH & LH, as well as hypothalamus release of GnRH
FSH surge purpose in menses
stimulates 4-6 follicles, 1 will mature
LH surge purpose in menses
ovulation
Corpus luteum fxn (2)
1)w/ LH stimulation it releases estrogen and progesterone
2)new menses cycle begins once it atrophies
There are 2 surges of estrogen what are the causes?
1)FSH effect on follicle
2)after ovulation LH stimulates the corpus luteum to release estrogen
3 phases of endometrium
1)FOLLICULAR PHASE- build up of endometrium b/c of estrogen stimualtion
2)LUTEAL PHASE- endometrium ready to be implanted b/c of estogen and progesterone
3)MENSES- endometrium sluffed off b/c no hormones to support it
If pregnancy occurs what keeps estrogen/progesterone high? (2)
1)Chorionic gonadotropin maintains CL to keep it releasing hormones
2)After 60 days, placenta produces the hormones
What is the signal for labor and delivery?
estrogen and progesterone fall off
____ & ____ are needed to maintain the endometrium
estrogen and progesterone
Estrogen biological activity (3)
1)changes that happen at puberty
2)secondary sexual characteristics
3)protective effect on bone and CV system
SERM? (2)
1)selective estrogen receptor modulators
2)act @ estrogen receptor to modulate estradiol activity
Progesterone biological activity (4)
1)axns are secondary to estrogen
2)needed for sexual development
3)menstrual regulation
4)pregnancy
2 types of estrogen receptors (ER) and where they are found?
1)ERalpha (reproductive tissue)
2)ERbeta (CV and bone)
ER is a ____ receptor
nuclear receptor
Estrogen mechanism (3)
1)estrogen binds to ER and a dimer is formed that recruits a coactivator
2)it is then able to bind DNA
3)acts as a transcription factor and elicits biological activity
Estrogen mechanism is the same as _____
progesterone's mechanism
Estrogen ADM?
A)readily absorbed
D)bound to sex hormone binding globulin and albumin
M)first pass metabolism in liver
Difference in D b/w synthetic estrogen and endogenous
synthetic are resistant to metabolism and are effective orally
Natural estrogen prototype
conjugated estrogens (premarin)
Orally active estrogens prototype
Ethinyl estradiol (estinyl)- used in OCs
Synthetic estrogens prototype and 2 properties
Diethylstillbesterol (stilphostrol)

nonsteroidal, orally active
Transdermal estrogen prototype
estradiol (estraderm)
Adverse effects of estrogen (5)
1)NAUSEA
2)fluid retention
3)CV (stroke, DVT)
4)breast cancer
5)chloasma (hyperpigmentation of skin/mask of pregnancy)
Antiestrogens
a)other name
b)basic mechanism
a)SERM
b)bind to ERalpha/beta and produce differing degrees of agonism/antagonism
Natural progestins prototype
a)dosage forms(2)
Progesterone acetate (Cyclin)
a)IM admin b/c poor GI absorption
b)gel for local intra-vaginal therapy
Synthetic progestins prototype
a)dosage form
b)difference from natural
Norethindrone (Norlutin)
a)oral activity
b)17 ethinyl to protect from 1st pass
T/F
a)The PR is a membrane bound receptor
b)progesterone acts at the estrogen receptor
c)Estradiol reacts w/ a cytoplasmic receptor to increased intracellular cAMP
a)false
b)false
c)false
T/F
1)gonadotropins are secreted in a pulsitile manner
2)Estrogens have an aromatic A ring
1)true
2)false?
2 principle classes of female sex hormones
1)estrogens
2)progestins
Estrogens fxn (2)
1)induce estrus
2)secondary sex characteristics
Progestins fxn (2)
1)reproduction
2)precursor to androgens, estrogens, adrenocorticoids
Where are sex steroids produced in females (2)
1)ovary
2)placenta
Where are sex steroids produced in males
testes
Where are sex steroids produced in both males and females (3)
1)adrenal cortex
2)hypothalamus
3)an. pituitary
A ring in testosterone vs estrogen
Both have an A ring but estrogen's is AROMATIC, testosterone's isnt
Estradiol to testosterone?
NOT possible, only the v.v. reaction
17-20 lyase fxn
converts 17alpha Hydroxypregnenolone to dehydroeplandrosterone via breaking off 2 carbons @ C17
Cholesterol to pregnenolone via...
break down of side chain of cholesterol
Biosynthesis of sex steroids begins w/...
cholesterol
17alpha hydroxylase fxn
pregnenolone to progesterone
_____ leads to male and female sex hormones (estradiol and testosterone)
Androstenedione****
Fxn of aromatase
aromatizes A ring of androstenedione
3 estrogens in the body
1)estradiol
2)estrone
3)estriol
Estradiol to estrone and v.v. via....
estradiol deH
Estrogen metabolism mainly occurs @...by...
A ring by adding OH onto the A ring via estrogen2/4 hydroxylase, making it metabolizable by COMT
Inactive metabolites of estrogen and how you get them
2/4 methoxy estrogens that are inactivated by COMT
Estrogens are eliminated from the body via...(3)
1)Glucuronide
2)sulfate
3)glutathione conjugates
thru the urine and this must all occur @ a free OH
Most potent endogenous androgen
5alpha dihydrotestosterone
Androgen metabolism occurs where? (and what is the major site) (4)
1)LIVER***
2)prostate gland
3)ovarian tissue
4)adipose tissue
How are androgens excreted in the urine (2)
via glucuronide and sulfate conjugations
Inactivation of androgens occurs when...
alpha/beta H @ C5 and keto group goes to alphaOH
____ was found in excess in Floyd Landis
androsterone
Structural features of estrogens (5)
1)aromatic A ring
2)phenolic OH @ C3
3)17beta OH
4)distance b/w 2 OH's is 8.55 angstroms
5)planar hydrophobic molecule
Which is more active and why? estrone vs. estradiol
estradiol b/c it has the 17beta OH and estrone does NOT
What can be done to estrogens to reduce their activity? (5)
1)insert OH @ C6,7,11
2)remove oxygen fxn from C3,17
3)epimerization of 17beta OH to alpha
4)unsaturation into B ring
5)enlargement of D ring
What can be done to increase estrogen activity
NOTHING
AAs @ the estrogen receptor AS that interact w/ estradiol (3)
1)histidine
2)glutamate
3)arginine
Female sex hormone derivatives are ____.... (3)
Estradiol derivatives
1)usually esterified to make orally active and incr half-life
2)or put on ethinyl @ C17
3)put ether on A ring